CHIR-99021 HCl 是一种有效的选择性 GSK-3α/β 抑制剂，IC50 为 10 nM 和 6.7 nM。CHIR-99021 HCl 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。CHIR-99021 HCl 还是一种有效的 Wnt/β-CATenin 信号通路激活剂。CHIR-99021 HCl 可增强小鼠和人类胚胎干细胞的自我更新。CHIR-99021 HCl 能诱导细胞Autophagy" style="display: inline; color: #c13a36">自噬 (Autophagy)。

CHIR-99021 HCl is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 HCl shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 HCl is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 HCl enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 HCl induces autophagy

CHIR-99021 HCl inhibits human GSK-3β with Ki values of 9.8 nM[1]. CHIR-99021 HCl is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites. In vitro kinase assays reveal that CHIR-99021 HCl specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[4]. In the presence of CHIR-99021 HCl the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR-99021 HCl with an IC50 of 4.9 μM[2].

In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) monohydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration[1]. Laduviglusib (2 mg/kg) monohydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR-99021 HCl treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. CHIR-99021 HCl treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h[5].

1797989-42-4

C22H19Cl3N8

501.8

Laduviglusib HCl;CT99021 HCl

DMSO:54.0 mg/mL (107.6 mM),Need ultrasonic
H2O:6.4 mg/mL (12.8 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years